Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.
Department of Genetics, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina, USA.
J Infect Dis. 2021 Aug 2;224(3):415-419. doi: 10.1093/infdis/jiab247.
Mutagenic ribonucleosides can act as broad-based antiviral agents. They are metabolized to the active ribonucleoside triphosphate form and concentrate in genomes of RNA viruses during viral replication. β-d-N4-hydroxycytidine (NHC, initial metabolite of molnupiravir) is >100-fold more active than ribavirin or favipiravir against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), with antiviral activity correlated to the level of mutagenesis in virion RNA. However, NHC also displays host mutational activity in an animal cell culture assay, consistent with RNA and DNA precursors sharing a common intermediate of a ribonucleoside diphosphate. These results indicate highly active mutagenic ribonucleosides may hold risk for the host.
诱变核苷可作为广谱抗病毒药物。它们在病毒复制过程中被代谢为活性核苷三磷酸形式,并在 RNA 病毒的基因组中浓缩。β-d-N4-羟基胞苷(NHC,莫那比拉韦的初始代谢物)对严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)的活性比利巴韦林或法匹拉韦高 100 多倍,其抗病毒活性与病毒 RNA 中的诱变水平相关。然而,NHC 在动物细胞培养测定中也显示出宿主突变活性,这与 RNA 和 DNA 前体共享一个核糖核苷二磷酸的共同中间产物一致。这些结果表明,高活性诱变核苷可能对宿主存在风险。